反应详情

温度

70 °C

A 50 mL flask was charged with 1-(3-(2-bromo-4-fluorophenoxy)-5-(3-methoxyphenylthio)pyridin-2-yl)thiourea (1.5 g, 3.12 mmol), triethylamine (0.740 mL, 5.31 mmol), tert-butyl 4-(2-bromoacetyl)piperidine-1-carboxylate (1.15 g, 3.75 mmol), and EtOH (25 mL). The reaction was heated to 70° C. for 2 hours. The reaction was partitioned between EtOAc and water. The organic layer was dried with sodium sulfate, filtered and concentrated. The residue was purified on silica (10% EtOAc in hexanes) to afford tert-butyl 4-(2-(3-(2-bromo-4-fluorophenoxy)-5-(3-methoxyphenylthio)pyridin-2-ylamino)thiazol-4-yl)piperidine-1-carboxylate (1.76 g, 82.0% yield).

1. customThe reaction was partitioned between EtOAc and water
2. dry with materialThe organic layer was dried with sodium sulfate
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified on silica (10% EtOAc in hexanes)